Aurora kinase/HDAC-IN-1

Name: Aurora kinase/HDAC-IN-1
Brand: TargetMol
SKU: T214435
Rating: 4.5 (1 reviews)

Catalog No. T214435 Copy Product Info

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Aurora kinase/HDAC-IN-1 is an orally active dual-target inhibitor of Aurora kinase and HDAC. It inhibits Aurora A (IC50 = 116 nM), Aurora B (IC50 = 225 nM), HDAC1 (IC50 = 164 nM), and HDAC2 (IC50 = 346 nM). This compound enhances histone acetylation (Ac-H3), inhibits phosphorylation of Aurora A and its downstream signaling, and induces apoptosis through G2/M phase arrest. In colorectal cancer cells HCT-116, Aurora kinase/HDAC-IN-1 shows significant antiproliferative activity with an IC50 of 30.2 nM and effectively suppresses tumor growth in HCT-116 colorectal cancer xenograft mouse models.

Aurora kinase/HDAC-IN-1

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Catalog No. T214435

Aurora kinase/HDAC-IN-1

Cas No. 2727102-12-5

Pack Size	Price	USA Stock	Global Stock	Quantity
10 mg	Inquiry	10-14 weeks	10-14 weeks
50 mg	Inquiry	10-14 weeks	10-14 weeks

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

Description	Aurora kinase/HDAC-IN-1 is an orally active dual-target inhibitor of Aurora kinase and HDAC. It inhibits Aurora A (IC50 = 116 nM), Aurora B (IC50 = 225 nM), HDAC1 (IC50 = 164 nM), and HDAC2 (IC50 = 346 nM). This compound enhances histone acetylation (Ac-H3), inhibits phosphorylation of Aurora A and its downstream signaling, and induces apoptosis through G2/M phase arrest. In colorectal cancer cells HCT-116, Aurora kinase/HDAC-IN-1 shows significant antiproliferative activity with an IC50 of 30.2 nM and effectively suppresses tumor growth in HCT-116 colorectal cancer xenograft mouse models.
Targets&IC50	Aurora A:116 nM
In vitro	Aurora kinase/HDAC-IN-1 (compound 6) (0.64 nM-10 μM; 72 hours) effectively inhibits the proliferation of HCT-116 and MIA PaCa-2 cells, with IC50 values of 30.2 nM and 42.8 nM, respectively. Aurora kinase/HDAC-IN-1 (30-120 nM; 24 hours) induces G2/M phase arrest in HCT-116 cells. This compound (30-120 nM; 48 hours) also triggers apoptosis in HCT-116 cells. Furthermore, after 72 hours at 30-120 nM, Aurora kinase/HDAC-IN-1 regulates Aurora/HDAC-related signaling in HCT-116 cells, promoting Ac-H3 and inhibiting Aurora A phosphorylation.
In vivo	Aurora kinase/HDAC-IN-1 (compound 6) administered orally at doses of 50-150 mg/kg/d once daily for 21 days effectively inhibits tumor growth in the HCT-116 colorectal cancer xenograft mouse model, achieving a tumor growth inhibition (TGI) of 71.8% at 150 mg/kg/d. This compound also demonstrates good oral bioavailability in mice (F = 23.2%).

Chemical Properties

Molecular Weight	449.51
Formula	C₂₂H₂₀FN₇OS
Cas No.	2727102-12-5
Smiles	O=C(NC1=CC=C(F)C=C1N)C2=CC=C(C=C2)CSC3=NC=CC(=N3)NC4=NNC(=C4)C

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc